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Preparation and biological evaluation of metronidazole derivatives with monoterpenes and eugenol
Author(s) -
Bkhaitan Majdi M.,
Alarjah Mohammed,
Mirza Agha Zeeshan,
Abdalla Ashraf N.,
ElSaid Hamdi M.,
Faidah Hani S.
Publication year - 2018
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13366
Subject(s) - eugenol , clostridium perfringens , carvacrol , chemistry , thymol , metronidazole , acetic acid , bacteria , microbiology and biotechnology , stereochemistry , chromatography , biochemistry , organic chemistry , antimicrobial , antibiotics , biology , essential oil , genetics
Two series of metronidazole derivatives (ester derivatives and ether derivatives) were prepared reacting metronidazole and its acetic acid oxidized form with menthol, thymol, carvacrol, and eugenol. Both series of compounds were tested in vitro against two strains of Helicobacter pylori (the ATCC 26695 and P12), and one strain of Clostridium ( Clostridium perfringens ). Most of the prepared compounds showed biological activity against the targeted bacteria. Compound 11 was highly active against all tested bacterial strains, especially against P12 with IC 50 0.0011 μM/ml. Compound 6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound 11 to test its selectivity for normal human fetal lung fibroblasts (MRC5), and it was found to be non‐toxic with IC 50 more than 50 μM/ml.